TABLE 3

In vitro activity of VBZ and HTBZ stereoisomers at dopamine, serotonin, and adrenergic receptors

Results expressed as percentage of control-specific binding: (tested compound-specific binding/control-specific binding) × 100. All compounds were tested at 1 or 10 μM final concentration, and results are an excerpt of a larger 80-target panel performed as an initial screen at Cerep (n = 2 for each compound at each target). Bolded results (>50%) indicate activity at target receptor; full dose response for these results are shown in Table 4.

Receptor Target	Cerep Broad Panel Screen (Excerpt)
Receptor Target	VBZ	R,R,R-HTBZ^{^a}	S,R,R-HTBZ	S,S,S-HTBZ/ R,S,S-HTBZ^{^b}
Serotonin5-HT_1A	26	17	69	96
Serotonin 5-HT_2A	1	−4	3	84
Serotonin 5-HT₇	4	3	80	98
Dopamine D₁	8	−6	−5	82
Dopamine D_2(s)	2	6	25	89

↵^a Major metabolite of VBZ.
↵^b For the purposes of the broad panel screen, the S,S,S- and R,S,S-metabolites were tested as a 50/50 mixture.